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    Platelet ADP receptor inhibitors
    5.
    发明授权
    Platelet ADP receptor inhibitors 失效
    血小板ADP受体抑制剂

    公开(公告)号：US06667306B1

    公开(公告)日：2003-12-23

    申请号：US09226103

    申请日：1999-01-07

    申请人： Alan M. Laibelman ,  Hans-Michael Jantzen ,  Pamela B. Conley ,  Larry J. Fretto ,  Robert M. Scarborough

    发明人： Alan M. Laibelman ,  Hans-Michael Jantzen ,  Pamela B. Conley ,  Larry J. Fretto ,  Robert M. Scarborough

    IPC分类号： C07D51314

    CPC分类号： C07D513/04

    摘要： The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.

    摘要翻译： 本发明涉及含有作为有效血小板ADP受体抑制剂的稠合杂环体系的式（I）化合物：式（I）中W是碳或氮，其中至少一个W是碳; Y是氮，氧或硫。 包括药学上可接受的盐的这些化合物可用于预防和/或治疗心血管疾病，特别是血栓形成相关的各种药物组合物。

    ANTIDOTES FOR FACTOR XA INHIBITORS AND METHODS OF USING THE SAME
    6.
    发明申请
    ANTIDOTES FOR FACTOR XA INHIBITORS AND METHODS OF USING THE SAME 有权
    因子XA抑制剂的抗体及其使用方法

    公开(公告)号：US20130129693A1

    公开(公告)日：2013-05-23

    申请号：US13591098

    申请日：2012-08-21

    申请人： Uma Sinha ,  Genmin Lu ,  Pamela B. Conley

    发明人： Uma Sinha ,  Genmin Lu ,  Pamela B. Conley

    IPC分类号： C07K14/745

    CPC分类号： C12N9/6432 ,  A61K38/482 ,  A61K38/4826 ,  A61K38/4833 ,  A61K38/4846 ,  A61K38/4853 ,  A61K39/00 ,  A61K47/60 ,  C12Y304/21006

    摘要： The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor X and factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of reversing anticoagulation, stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.

    摘要翻译： 本发明涉及靶向因子Xa的抗凝剂的解毒剂。 解毒剂是与因子Xa抑制剂结合的因子X和因子Xa蛋白衍生物，从而基本上中和它们，但不组装到凝血酶原酶复合物中。 本文所述的衍生物缺乏或具有降低的内在凝结剂活性。 本文公开的是使用因子Xa抑制剂正在进行抗凝治疗的患者中的抗凝，停止或预防出血的方法。

    TARGETED DELIVERY AND EXPRESSION OF PROCOAGULANT HEMOSTATIC ACTIVITY
    9.
    发明申请
    TARGETED DELIVERY AND EXPRESSION OF PROCOAGULANT HEMOSTATIC ACTIVITY 审中-公开
    目标交付和表达程序化学活动

    公开(公告)号：US20080241233A1

    公开(公告)日：2008-10-02

    申请号：US12057100

    申请日：2008-03-27

    申请人： Peter J. Sims ,  Pamela B. Conley ,  Peng Luan ,  David R. Phillips

    发明人： Peter J. Sims ,  Pamela B. Conley ,  Peng Luan ,  David R. Phillips

    IPC分类号： A61K9/127 ,  A61K38/02 ,  A61K39/395 ,  A61K38/17 ,  A61K38/43

    CPC分类号： A61K9/1271 ,  A61K9/1272 ,  A61K31/685 ,  A61K38/177 ,  A61K38/46 ,  A61K47/6843 ,  A61K47/6913 ,  A61K2300/00

    摘要： A platelet substitute consisting of large unilamellar lipid vesicles that contain phosphatidylserine or another procoagulant (clot-promoting) phospholipid, a protein that has binding affinity for collagen or other component of the vessel wall that becomes exposed upon vessel injury, and/or a phospholipid scramblase, has been developed. This platelet substitute provides a means for selectively delivering procoagulant phospholipids and/or fatty acids to the site of vessel injury through targeted adherence to collagen or other component exposed upon vessel injury. These are particularly effective due to the combination of targeting procoagulant vesicles to a site of injury, and triggered exposure of phosphatidylserine (PS) on the surface.

    摘要翻译： 包含含有磷脂酰丝氨酸或另一促凝血素（促凝血素）磷脂的大单层脂质囊泡的血小板替代物，对血管损伤时暴露于血管壁的胶原蛋白或其他成分具有结合亲和力的蛋白质和/或磷脂类 ，已经开发。 该血小板替代物提供了通过靶向粘附到血管损伤时暴露于胶原或其它组分的选择性地将促凝血磷脂和/或脂肪酸输送到血管损伤部位的手段。 由于靶向促凝血小泡与损伤部位的结合，并且触发表面上的磷脂酰丝氨酸（PS）的暴露，这些是特别有效的。